AMLODIPINE

What is Amlodipine?

Amlodipine is a medication belonging to the class of drugs known as calcium channel blockers.

It is primarily used for the treatment of hypertension, also known as high blood pressure.

Amlodipine works by blocking the entry of calcium into smooth muscle cells of the arteries, leading to relaxation and dilation of the blood vessels, which results in decreased peripheral resistance and lower blood pressure.

Amlodipine is commonly prescribed as an oral tablet or capsule, and it is typically taken once daily. 

It is available in various strengths, including 2.5 mg, 5 mg, and 10 mg.

What is amlodipine used for?

Hypertension – It helps lower blood pressure levels. By reducing blood pressure, it can effectively decrease the risk of serious cardiovascular events such as strokes and heart attacks, both fatal and nonfatal in nature.

Angina (chest pain) – This medication is commonly used to treat chronic stable angina, and vasospastic angina (also known as Prinzmetal or variant angina). Call a doctor immediately. 

Coronary Artery Disease – It is used in angiographically documented coronary artery disease (CAD) in patients who do not have heart failure or an ejection fraction (EF) of less than 40%.

Dosage

Disclaimer!

⇒ Hypertension

» For adults

The recommended initial Dosage of this medication is 5 mg per day taken orally.

It may be increased by 2.5 mg daily every 7-14 days, but it should not exceed a maximum daily dose of 10 mg for maintenance.

The dosage should be adjusted based on the individual’s blood pressure goals, as determined by their healthcare provider.

⇒ Angina (Chest pain)

» For adults

The typical initial dosage of this medication is 5-10 mg per day, taken orally.

Once the initial dosage is established, the recommended maintenance dosage is 10 mg per day, also taken orally.

It’s important to follow the specific dosing instructions provided by your healthcare provider for optimal results.

» For elderly patients

The typical initial dosage of this medication is 2.5-5 mg per day, taken orally.

The dosage may be increased by 2.5 mg per day every 7-14 days, but should not exceed a maximum daily dose of 10 mg for maintenance.

The recommended maintenance dosage for elderly patients is 5-10 mg per day, taken orally.

It’s important to closely monitor elderly patients for any potential side effects or interactions with other medications they may be taking, and to consult with a healthcare provider for appropriate dosage adjustments based on their individual health status.

» For children under 6 years

This medication has not been established as safe and effective for the treatment of hypertension in children under the age of 6 years.

It is important to consult with a healthcare provider for appropriate treatment options for pediatric patients with hypertension, as their safety and efficacy may not be well-documented for this age group.

» For 6-17 years

The recommended dosage of this medication is typically 2.5-5 mg per day taken orally.

It’s worth noting that doses above 5 mg per day have not been extensively studied in this age group, and therefore caution should be exercised when considering higher doses.

⇒ Coronary Artery Disease

» For adults

The typical initial dosage of this medication is 5-10 mg per day, taken orally.

Once the initial dosage is established, the recommended maintenance dosage is 10 mg per day, also taken orally.

It’s important to follow the specific dosing instructions provided by your healthcare provider for optimal results.

» For elderly patients

The recommended initial dosage of this medication is 2.5-10 mg per day, taken orally.

After the initial dosage is established, the recommended maintenance dosage is 10 mg per day, taken orally.

⇒ Dosage Modifications

Renal Impairment:

The way amlodipine is processed in the body (pharmacokinetics) is not significantly affected by renal impairment, which means that no dosage adjustment is typically necessary for patients with kidney problems.

Hepatic Impairment:

For patients with liver impairment, it may be necessary to start with a lower initial dose of amlodipine. Consider beginning with a dose of 2.5 mg per day taken orally (by mouth).

If you are currently taking amlodipine, you may have questions like Can I stop using amlodipine any time? The answer is NO. If you have been using this medication consistently for a few weeks, it is essential not to abruptly discontinue using it.

Abruptly stopping the medication can result in a recurrence or worsening of your chest pain or high blood pressure.

It is advisable to consult your doctor to determine the best way to gradually reduce the dosage before discontinuing it entirely.

This approach can help minimize the risk of negative effects when stopping the medication.

So, How long does it take for amlodipine to lower blood pressure? Amlodipine typically begins to take effect on the day that you start taking it, but it may take a few weeks before it reaches its full efficacy.

If you are using amlodipine to manage high blood pressure, it is possible that you may not experience any noticeable symptoms.

If you are more curious about Why take amlodipine at bedtime?

There are several reasons why taking amlodipine at bedtime may be beneficial:

⇒ Peak activity of the renin-angiotensin system during sleep: The renin-angiotensin system is a body system that strongly affects blood pressure, and it has its peak activity during sleep. Taking amlodipine at bedtime may align with this peak activity and result in better blood pressure control. Read the research article here.

⇒ Circadian rhythms: The body’s chemistry varies between night and daytime due to circadian rhythms. Taking amlodipine at bedtime may take advantage of these differences in body chemistry at night and potentially lead to more effective blood pressure control. Read the research article here.

⇒ More even blood levels and effectiveness: Taking amlodipine at the same time every day, preferably at bedtime, may result in more consistent blood levels of the medication, leading to better effectiveness in managing blood pressure.

⇒ 24-hour effect with one dose: Amlodipine has been shown to keep blood pressure low for the entire 24-hour period when taken once a day. Taking it at bedtime may ensure that the medication is effective throughout the night and the following day, providing continuous blood pressure control.

How long does amlodipine stay in your system? If amlodipine is taken daily, then its effects can last for up to 24 hours. As long as amlodipine is taken regularly as prescribed by a doctor, its effects should continue to last. If a patient is advised by their doctor to stop taking amlodipine, the medication can remain in their system for approximately 10 days after the last dose.

What is the most common side effect of amlodipine or What are the dangers of taking amlodipine?

Amlodipine is generally considered safe for the heart when used as prescribed by a healthcare professional.

⇒ The most common side effects of amlodipine are:

Dizziness: Amlodipine can cause dizziness, which may be mild or severe and may affect balance and coordination.

Peripheral edema: Amlodipine may cause swelling in the ankles, feet, or hands due to fluid retention, which is usually mild to moderate in severity.

Flushing: Amlodipine can cause flushing, temporary redness, and warmth of the skin, usually on the face and neck.

Headache: Amlodipine may cause headaches, which can range from mild to severe and may be persistent or intermittent.

In most cases, the common side effects of amlodipine are mild and temporary, and they go away on their own as your body adjusts to the medication. However, if your symptoms persist or become severe, you should talk to your healthcare provider.

⇒ The most serious side effects of amlodipine are:

Hypotension: Amlodipine can cause low blood pressure, which may result in symptoms such as dizziness, fainting, or weakness.

Cardiac effects: Amlodipine may rarely cause serious cardiac effects, such as irregular heartbeat, chest pain, or heart attack.

Allergic reactions: Amlodipine may cause rare but serious allergic reactions, including rash, itching, swelling, difficulty breathing, and severe dizziness.

If serious side effects of amlodipine occur, it is important to seek immediate medical attention by calling emergency services (such as 911 in the USA, 999 in the UK, and 108 or 112 in India) or going to the nearest hospital right away.

In the USA, serious side effects of amlodipine can be reported to the Food and Drug Administration (FDA) by using the FDA’s MedWatch Adverse Event Reporting program. The program can be accessed online or by calling 1-800-FDA-1088 (1-800-332-1088). Healthcare providers are required to report serious adverse events to the FDA, but patients and caregivers can also report adverse events through the program.

Can amlodipine affect kidneys? There are also some concerns about the effects of amlodipine on the kidneys. While amlodipine has been found to have protective effects against renal damage in some studies, there have been reports of decreased urine output in some patients taking amlodipine, which may raise concerns about its impact on kidney function.

It is important to discuss any concerns or pre-existing conditions related to kidney function with a healthcare professional before starting or changing any medication regimen, including amlodipine.

What should you avoid when taking amlodipine?

The bioavailability of all Ca2+ channel blockers is reduced, in some cases markedly, by first-pass metabolism by CYP3A4 enzymes in the intestinal epithelium and the liver. This has two consequences:

⇒ The bioavailability of these drugs may be increased by strong inhibitors of CYP3A4, such as macrolide and imidazole antibiotics, antiretroviral agents, and grapefruit juice.

⇒ Bioavailability is reduced by inducers of CYP3A4, such as rifampin, carbamazepine, and hypericum (St. John’s wort).

⇒ Some Ca2+ channel blockers (particularly verapamil) are strong CYP3A4 inhibitors and cause clinically relevant drug interactions with other CYP3A4 substrates, such as simvastatin and atorvastatin.

Precautions and Warnings

When taking amlodipine, a medication used to treat high blood pressure, there are some precautions and things to avoid to ensure its safe and effective use.

Follow up with your doctor regularly: It is essential to have regular check-ups with your doctor to monitor your progress and make sure the medication is working effectively. Blood tests may be needed to check for any unwanted effects.

Avoid getting up too fast from sitting or lying position: Amlodipine may cause dizziness, so it is important to get up slowly and steady yourself to prevent a fall.

Be cautious with other medications: Some medicines may not mix well with amlodipine, so it’s crucial to talk to your doctor about all the medications you are taking. Certain medications, such as other blood pressure-lowering drugs, may cause your blood pressure to drop too much when taken with amlodipine.

Avoid stopping or changing doses without consulting your doctor: Amlodipine should be taken as prescribed by your doctor, and any changes to the dosage or stopping the medication should be done only under the guidance of a healthcare professional.

Be cautious with grapefruit juice: Although there are no specific food restrictions with amlodipine, it is advised to be cautious with grapefruit juice as it may affect the pharmacokinetics of amlodipine.

Follow your doctor’s instructions: It is crucial to follow your doctor’s instructions and take amlodipine as prescribed. Do not exceed the recommended dosage or duration of use without consulting your healthcare provider.

It is important to note that this is not an exhaustive list, and you should always consult your healthcare provider for personalized medical advice regarding your specific condition and medication regimen.

Who Cannot take amlodipine?

Individuals who have had an allergic reaction to amlodipine or any other medicine should not take amlodipine.

Individuals with liver or kidney disease should inform their doctor before taking amlodipine to ensure it is safe for them.

Individuals with heart failure or those who have recently had a heart attack should inform their doctor before taking amlodipine.

Individuals who have a heart valve problem called aortic stenosis should not take amlodipine or should inform their doctor before taking it to ensure it is safe for them.

Pregnant individuals or those planning to become pregnant should inform their doctor before taking amlodipine as its safety during pregnancy is not known.

What is the best alternative to amlodipine?

First of all, It’s important to consult with a healthcare provider to determine the best alternative to amlodipine based on individual health conditions and considerations.

There are several alternatives to amlodipine, which is a medication used to treat high blood pressure.

These alternatives include other calcium channel blockers such as nifedipine, diltiazem, or verapamil as well as other dihydropyridine calcium channel blockers like felodipine, lercanidipine, and barnidipine.

Lisinopril, an angiotensin-converting enzyme (ACE) inhibitor, may also be a good alternative for people who are allergic or sensitive to amlodipine, or for those at increased risk of heart attack or heart failure.

Thiazide diuretics, such as chlorthalidone and hydrochlorothiazide, are another option for blood pressure management.

The ACE inhibitors perindopril proved superior to the combination of the β blocker atenolol and hydrochlorothiazide (Dahlof et al., 2005), and amlodipine was superior to hydrochlorothiazide as the combination partner for the ACEI benazepril (Jamerson et al., 2008).

References

Dahlof B, et al. Prevention of cardiovascular events with an antihypertensive regimen of amlodipine adding perindopril as required versus atenolol adding bendroflumethiazide as required, in the AngloScandinavian Cardiac Outcomes Trial-Blood Pressure Lowering Arm (ASCOT-BPLA): a multicentre randomised controlled trial. Lancet, 2005, 366:895–906

Jamerson K, Weber MA, Bakris GL, Dahlöf B, Pitt B, Shi V, Hester A, Gupte J, Gatlin M, Velazquez EJ. Benazepril plus amlodipine or hydrochlorothiazide for hypertension in high-risk patients. New England Journal of Medicine. 2008 Dec 4;359(23):2417-28.

Lacourciere Y, et al. Antihypertensive effects of amlodipine and hydrochlorothiazide in elderly patients with ambulatory hypertension. Am J Hypertens, 1995, 8:1154–1159.

Meredith PA, Elliott HL. Clinical pharmacokinetics of amlodipine. Clinical pharmacokinetics. 1992 Jan;22(1):22-31.

Burges RA, Dodd MG, Gardiner DG. Pharmacologic profile of amlodipine. The American Journal of Cardiology. 1989 Nov 7;64(17):I10-20.

Beresford AP, McGibney D, Humphrey MJ, Macrae PV, Stopher DA. Metabolism and kinetics of amlodipine in man. Xenobiotica. 1988 Jan 1;18(2):245-54.

Kloner RA, Sowers JR, DiBona GF, Gaffney M, Marilee W, for list of Members SA, Amlodipine Cardiovascular Community Trial Study Group. Sex-and age-related antihypertensive effects of amlodipine. The American journal of cardiology. 1996 Apr 1;77(9):713-22.